celecoxib (Celebrex)
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Introduction
Tradename: Celebrex. Molecular formula: C17H14F3N3O2S.
1st generic FDA-approved May 30, 2014[14]
Indications
- pain, including acute pain & inflammatory conditions
- dysmenorrhea[5]
- inhibition of colonic polyps
- adjunctive therapy for familial adenomatous polyposis (FAP)
Contraindications
- allergy to sulfonamides[7]
- severe hepatic impairment or active liver disease (Canada)
- avoid in patients with cardiovascular risk factors
Dosage
- 100-200 mg BID or 200 mg QD
- 100 mg TID (acute crystalline arthritis)
Tabs: 100 & 200 mg.
Pharmacokinetics
- plasma protein binding 97%
- volume of distribution 400 L/kg
- hepatic metabolism occurs via cyt P450 2C9
- inhibits cyt P450 2D6
- elimination 1/2life is 11.2 hours (fasting)
- 57% eliminated in feces; 27% eliminated in urine
elimination via liver
1/2life = 11-16 hours
protein binding = 97 %
Monitor
- liver function tests periodically[11]
Adverse effects
- gastrointestinal
- abdominal pain
- diarrhea
- flatulence
- GI bleed, gastritis, peptic ulcer
- GI complications less frequent than with non-selective NSAIDs[6]
- peripheral edema (less than rofecoxib (Vioxx)[8])
- pharyngitis
- rhinitis
- nephrotoxicity[3]
- impaired renal physiologic responses similar to non-selective NSAIDs
- sulfonamide derivative: may cause allergies in patients with sulfa allergies[3]
- myocardial infarction (MI)
- risk of stroke comparable to ibuprofen & naproxen[15]
- aseptic meningitis (within 2 weeks)[6]; recovery with stopping drug
- ocular effects
- blurred vision, cataracts, conjunctivitis, conjunctival hemorrhage, eye pain, glaucoma, vitreous floaters
- adverse effects might be caused by alteration of retinal blood flow &/or inflammation resulting from secretion of the medication in tears
- stopping celecoxib should resolve most ocular side effects within 72 hours
- drug adverse effects of NSAIDs
- drug adverse effects of COX-2-specific inhibitors
- drug adverse effects of sulfonamides
Drug interactions
- any drug which inhibits cyt P450 2C9 can increase celecoxib levels
- any drug which induces cyt P450 2C9 can diminish celecoxib levels
- may increase levels of drugs metabolized by cyt P450 2D6
- drug interaction(s) anticonvulsants with anti-bacterial agents
- drug interaction(s) of antibiotics with warfarin
- drug interaction(s) of cholinesterase inhibitors with NSAIDs
- drug interaction(s) of lithium carbonate with NSAIDs
- drug interaction(s) of NSAIDs with oral contraceptive
- drug interaction(s) of NSAIDs with SSRIs
- drug interaction(s) of NSAIDs with antidepressants
- drug interaction(s) of aspirin with NSAIDs
- drug interaction(s) of apixaban with NSAIDs
- drug interaction(s) of warfarin with NSAIDs
- drug interaction(s) of NSAIDs with beta blockers
- drug interaction(s) of NSAIDs with ARBs
- drug interaction(s) of coxib with SSRI
- drug interaction(s) of NSAIDs with aldosterone antagonis
- drug interaction(s) of NSAIDs with glucocorticoid
- drug interaction(s) of NSAIDs, diuretics & angiotensin II receptor antagonists
- drug interaction(s) of NSAIDs, diuretics & ACE inhibitors
- drug interaction(s) of NSAIDs with ACE inhibitors
- drug interaction(s) of NSAIDs & antihypertensives
- drug interaction(s) of NSAIDs & loop diuretics
- drug interaction(s) of NSAIDs & aspirin
Laboratory
Mechanism of action
- selectively inhibits cyclo-oxygenase-2 (COX-2)
- at therapeutic concentrations in humans, celcoxib does not inhibit COX-1
- does NOT inhibit platelet aggregation
More general terms
Additional terms
Component of
References
- ↑ Searle-Pfizer package insert
- ↑ Prescriber's Letter 7(2):11, Feb. 2000
- ↑ 3.0 3.1 3.2 Prescriber's Letter 7(10):55 2000
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 5.0 5.1 Prescriber's Letter 8(11):61 2001
- ↑ 6.0 6.1 6.2 6.3 Prescriber's Letter 9(5):26 2002
- ↑ 7.0 7.1 Prescriber's Letter 11(7):42 2004 Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=200702&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 8.0 8.1 Journal Watch 24(14):109, 2004 Mamdani M, Juurlink DN, Lee DS, Rochon PA, Kopp A, Naglie G, Austin PC, Laupacis A, Stukel TA. Cyclo-oxygenase-2 inhibitors versus non-selective non-steroidal anti-inflammatory drugs and congestive heart failure outcomes in elderly patients: a population-based cohort study. Lancet. 2004 May 29;363(9423):1751-6. PMID: https://www.ncbi.nlm.nih.gov/pubmed/15172772
- ↑ 9.0 9.1 9.2 Associated Press, Netscape 12/17/04 sites NCI study conducted for Pfizer
- ↑ 10.0 10.1 Prescriber's Letter 13(10): 2006 Cardiovascular Risks of NSAIDs and COX-2 Inhibitors Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=221003&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 11.0 11.1 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Cryer B et al. GI-REASONS: A novel 6-month, prospective, randomized, open-label, blinded endpoint (PROBE) trial. Am J Gastroenterol 2013 Mar; 108:392. PMID: https://www.ncbi.nlm.nih.gov/pubmed/23399552
- ↑ 13.0 13.1 Medical Knowledge Self Assessment Program (MKSAP) 16 American College of Physicians, Philadelphia 2012
- ↑ 14.0 14.1 FDA News Release. May 30, 2014 FDA approves first generic versions of celecoxib. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm399428.htm
- ↑ 15.0 15.1 15.2 Nissen SE, Yeomans ND, Solomon DH et al Cardiovascular Safety of Celecoxib, Naproxen, or Ibuprofen for Arthritis. N Engl J Med. Nov 13, 2016 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27959716 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1611593
FitzGerald GA. ImPRECISION: Limitations to interpretation of a large randomized clinical trial. Circulation 2016 Nov 13; <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27840335 <Internet> http://circ.ahajournals.org/content/early/2016/11/11/CIRCULATIONAHA.116.026324 - ↑ 16.0 16.1 Therapeutics Letter #108. Therapeutics Initiative Drugs to Avoid. http://www.ti.ubc.ca/2018/01/04/108-drugs-avoid/
- ↑ 17.0 17.1 Elia J, Sadoughi S, Saitz R. Celecoxib Gets Partial Exoneration from FDA Panels Physician's First Watch, April 26, 2018 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org
Stein R Celebrex As Safe As Ibuprofen And Naproxen, FDA Advisers Say. Health News from NPR. April 25, 2018 https://www.npr.org/sections/health-shots/2018/04/25/605226604/fda-panel-affirms-safety-of-painkiller-celebrex